Tachykinin is a generic term for a group of neuropeptides. Substance P (SP), neurokinin A (NK-A) and neurokinin B (NK-B) are known in mammals, and these peptides are known to bind to the corresponding receptors (neurokinin-1 (NK-1), neurokinin-2 (NK-2) and neurokinin-3 (NK-3)) that exist in a living body and thereby to exhibit various biological activities.
Of such neuropeptides, SP has the longest history and has been studied in detail. In 1931, the existence of SP in the extract from equine intestines was confirmed, and in 1971, its structure was determined. SP is a peptide consisting of 11 amino acids.
SP is broadly distributed over the central and peripheral nervous systems, and has various physiological activities such as vasodilation, enhancement of vascular permeability, contraction of smooth muscles, excitation of neurons, salivation, enhancement of diuresis, immunological enhancement and the like, in addition to the function as a transmitter substance for primary sensory neurons. In particular, it is known that SP released from the terminal of the spinal (dorsal) horn due to a pain impulse transmits the information of pain to secondary neurons, and that SP released from the peripheral terminal induces an inflammatory response in the receptor thereof. Thus, it is considered that SP is involved in various disorders (e.g., pain, headache, particularly migraine, Alzheimer's disease, multiple sclerosis, cardiovascular modulation, chronic inflammatory diseases such as chronic rheumatic arthritis, respiratory diseases including asthma or allergic rhinitis, intestinal inflammatory diseases including ulcerative colitis and Crohn's disease, ocular damage and ocular inflammatory diseases, proliferative vitreoretinopathy, an irritable bowel syndrome, urinary frequency, psychosis, vomiting, etc.) [see, for example, Physiological Reviews, Vol. 73, pp. 229-308 (1993); Journal of Autonomic Pharmacology, Vol. 13, pp. 23-93 (1993)].
At present, as a compound having an SP receptor antagonistic action, WO03/057668 describes a compound represented by the formula
wherein each of rings A and B is an optionally substituted aromatic ring, or rings A and B may be bonded to each other to form a ring by linking bonds or substituents thereof; ring C is a nitrogenous saturated heterocyclic ring optionally having substituents besides oxo (excluding 2,3-dioxopyrrolidine ring); R1 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and  is a single bond or a double bond, or a salt thereof.
In addition, WO03/101964 describes a compound represented by the formula
wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, R1 is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group, X is an oxygen atom or an optionally substituted imino group, Z is an optionally substituted methylene group, Ring A is a further optionally substituted piperidine ring, and Ring B is an optionally substituted aromatic ring, provided that when Z is a methylene group substituted with an oxo group, R1 is not a methyl group, and when Z is a methylene group substituted with a methyl group, Ring B is a substituted aromatic ring, or a salt thereof.
Furthermore, WO2005/068427 describes a compound represented by the formula
wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B and ring C are each an aromatic ring optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group or a heterocyclic group optionally having substituent(s), Z is an optionally halogenated C1-6 alkyl group, Y is a methylene group optionally having substituent(s), m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and  is a single bond or a double bond, or a salt thereof.
Moreover, WO2006/030975 describes a compound represented by the formula
wherein Ar is an aryl group optionally having substituent(s), R is a C1-6 alkyl group, R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group or a heterocyclic group optionally having substituent(s), X is an oxygen atom or an imino group optionally having a substituent, ring A is a piperidine ring optionally further having substituent(s), and ring B is a benzene ring having substituent(s), or a salt thereof.
In addition, WO2006/115286 describes an optically active compound represented by the formula
wherein ring A is an optionally further substituted piperidine ring, R1 is a hydrogen atom or a group represented by R1′—C(═O)— wherein R1′ is(i) an optionally substituted 5- or 6-membered nitrogen-containing heterocyclic group,(ii) an optionally substituted C1-6 alkyl group, or(iii) an optionally substituted C1-6 alkoxy group, andR2 is a hydrogen atom, an optionally substituted C1-3 alkyl group, or a C3-6 cycloalkyl group, excluding cis-1-(methoxyacetyl)-N-[2-methoxy-5-[5-(trifluoromethyl)-1H-tetrazol-1-yl]benzyl]-3-phenyl-4-piperidinamine and cis-1-[(1-acetyl-4-piperidinyl)carbonyl]-N-[2-methoxy-5-[5-(trifluoromethyl)-H-tetrazol-1-yl]benzyl]-3-phenyl-4-piperidinamine, or a salt thereof.
Moreover, WO2007/015588 describes a compound represented by the formula
wherein Ar is a phenyl group optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group or a heterocyclic group optionally having substituent(s), R2 is a hydrogen atom, a C1-6 alkyl group optionally having substituent(s) or a C3-6 cycloalkyl group optionally having substituent(s), Z is a methylene group optionally having a C1-6 alkyl group, ring A is a piperidine ring optionally further having substituent(s), ring B and ring C are benzene rings optionally further having substituent(s), and R2 optionally forms a ring together with the adjacent substituent on the ring B, excluding the compounds represented by the formula:
and the formula:
or a salt thereof.
Furthermore, WO2007/089031 describes a compound represented by the formula
whereinAr is a phenyl group optionally having substituent(s),R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group or a heterocyclic group optionally having substituent(s),Z is a methylene group optionally having C1-6 alkyl group(s), ring A is a piperidine ring optionally further having substituent(s), andB is a monocyclic aromatic heterocyclic group optionally having substituent(s) (substituents of the monocyclic aromatic heterocycle may be bonded to each other to form a ring), or a salt thereof.
Also, WO2008/133344 describes a compound represented by the formula
wherein R1 is carbamoylmethyl, methylsulfonylethylcarbonyl and the like; R2 is methyl or cyclopropyl; R3 is a hydrogen atom or methyl; R4 is a chlorine atom or trifluoromethyl; R5 is a chlorine atom or trifluoromethyl; and a group represented by the formula
is a group represented by the formula
wherein R6 is a hydrogen atom, methyl, ethyl or isopropyl; R7 is a hydrogen atom, methyl or a chlorine atom; and R8 is a hydrogen atom, a fluorine atom, a chlorine atom or methyl, or 3-methylthiophen-2-yl, or a salt thereof.
WO2009/072643 describes a compound represented by the formula
wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B is an aromatic ring optionally having substituent(s), ring C is a cyclic group optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group, a heterocyclic group optionally having substituent(s) or an amino group optionally having substituent(s), R2 is an optionally halogenated C1-6 alkyl group, m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, andis a single bond or a double bond, excluding N-[(rac.)-(3R,4R)-1-benzyl-4-phenylpiperidin-3-yl]-N-isopropyl-4-methoxy-3-(3-methoxypropoxy)benzamide, N-isopropyl-4-methoxy-3-(3-methoxypropoxy)-N-[(rac.)-(3R,4R)-4-phenylpiperidin-3-yl]benzamide, N-isopropyl-4-methoxy-3-(3-methoxypropoxy)-N-[(rac.)-(3R,4R)-4-(3-(methylsulfonyl)amino-phenyl)-piperidin-3-yl]benzamide, N-isopropyl-[(rac.)-(3R,4R)-4-[1,1′-biphenyl]-3-yl-3-piperidinyl]-4-methoxy-3-(3-methoxypropoxy)benzamide, N-ethyl-[(rac.)-(3R,4R)-4-[1,1′-biphenyl]-3-yl-3-piperidinyl]-4-methoxy-3-(3-methoxypropoxy)benzamide, N-propyl-[(rac.)-(3R,4R)-4-[1,1′-biphenyl]-3-yl-3-piperidinyl]-4-methoxy-3-(3-methoxypropoxy)benzamide, N-ethyl-[(rac.)-(3R,4R)-4-[3-[(3,5-dimethoxyphenyl)methoxy]phenyl]-3-piperidinyl]-4-methoxy-3-(3-methoxypropoxy)benzamide and 4-methoxy-3-(3-methoxypropoxy)-N-isopropyl-N-[(rac.)-4-(4-phenyl-2-oxazolyl)-3-piperidinyl]benzamide, or a salt thereof.
In addition, US Patent Application Publication No. 2005/0256164 describes the following compound
wherein m, n and s are each independently 0 or 1, L is —O— or —NR4—, R1 and R2 are each independently hydrogen, aryl, heteroaryl, (C1-C6)alkyl, (C1-C6)alkyl-heteroaryl and the like, R3 is hydrogen and the like, and X and Y are each independently hydrogen, (C1-C6)alkyl and the like, as a NK-1 and NK-3 receptor antagonist.
Xenobiotica (2006), 36(2/3), 235-258, describes the following compound
as a receptor antagonist for tachykinin, SP, NK-A or NK-B.
In addition, WO2004/111000 describes a compound represented by the following formula (I)
wherein—X— is —NH— or —O—,Y is
whereinR3, R4 and R5 are independently hydrogen, lower alkyl, mono(or di or tri)halo(lower)alkyl and the like; andR6 and R7 are each independently hydrogen or lower alkoxy, and the like,—Z— is a bond or —CH(R11)— wherein R11 is hydrogen or lower alkyl,R1 and R2 are independently hydrogen or lower alkyl, or in combination form oxo,R8 is hydrogen, (5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl or an amino protecting group,R9 and R10 are hydrogen, halogen and the like, or a salt thereof, as a compound having a tachykinin receptor antagonistic action.
In addition, a selective peptidic antagonist of NK-2 receptor is known (Br. J. Pharmacol., 1990, vol. 100, pages 588-592 and WO97/31941). However, these known peptidic NK-2 antagonists have low activity and are metabolically unstable. Therefore, it is difficult to provide them as practical prophylactic drugs or therapeutic drugs.
As the selective non-peptidic NK-2 receptor antagonists, SR 48968 (Brit. J. Pharmacol. 1992, vol. 105, page 77), GR-159897 (Bioorg. Med. Chem. Lett. 1994, vol. 4, page 1951), CP 96345 (Science, 1991, vol. 251, page 435), RP 67580 (Proc. Nat. Acad. Sci. 1991, vol. 88, page 10208), ZD 7944 (Abstracts of Papers, Part 1, 214th NATIONAL Meeting of the American Chemical Society, Las Vegas, Nev., Sep. 7-11, 1997, MEDI 264), WO02/38547, WO02/38548, WO02/083663, WO02/083664 and the like are known.
In addition, as the quinoline derivatives to be condensed with a nitrogen-containing heterocycle, the compounds described in J. Org. Chem., 2000, 65, 655-666; J. Org. Chem., 2003, 68, 442-451; Org. Lett., 2001, 3, 2189-2191; Org. Lett., 2001, 3, 4217-4220; Tetrahedron 57, 2001, 5615-5624; Tetrahedron Letters 40, 1999, 1215-1218; Tetrahedron Letters 40, 1999, 3339-3342; Heterocycles, 2004, 63, 1685-1712 and U.S. Pat. No. 5,288,725 and the like are known. Furthermore, WO05/105802 is known.
JP-A-2007-277231 and WO 2006/030984 describe, as synthesis intermediates for tachykinin receptor antagonist, the following compounds.

In addition, WO2004/111000 discloses, as synthesis intermediates for tachykinin receptor antagonist, the following compounds.

In addition, WO2000/018403 discloses, as synthesis intermediates for NK1 receptor antagonist, the following compounds.

In addition, US 2007/0167433 describes, as synthesis intermediates for β-secretase, cathepsin D, plasmepsin II and/or HIV protease inhibitor, and WO2006/005741 describes, as synthesis intermediates for rennin inhibitory substance, the following compounds.

In addition, WO2003/045920 discloses, as melanin coagulation hormone receptor (MCH-1R) antagonists, the following compounds.

In addition, WO2002/088101 discloses, as a BACE (β amyloid precursor protease) inhibitor, the following compound.

Moreover, the relationship between NK-3 receptor and central nervous system diseases, particularly depression, has been pointed out (Pharmacol. Biochem. Behav., 83 (2006), 533-539; Nature Rev. Drug Discov., 4, 967-975, 2005). Therefore, a compound showing an NK-3 receptor binding action is considered to be promising as a therapeutic drug for the central nervous system diseases.